alisertib + endocrine therapy

Alisertib is an investigational, orally administered, selective small molecule inhibitor of Aurora kinase A. In the context of Puma Biotechnology's clinical development program, it is being evaluated in combination with various endocrine therapies—including aromatase inhibitors (anastrozole, letrozole, exemestane), selective estrogen receptor modulators (tamoxifen), or selective estrogen receptor degraders (fulvestrant). The mechanism of action for alisertib involves ATP-competitive and reversible inhibition of Aurora kinase A, which disrupts mitosis and induces apoptosis in rapidly proliferating tumor cells. This combination therapy is specifically targeted at patients with hormone receptor-positive (HR+), HER2-negative recurrent or metastatic breast cancer who have progressed on CDK 4/6 inhibitors and prior lines of endocrine therapy. The Phase II ALISCA-Breast1 trial is currently optimizing the dose of alisertib when used in this combined regimen.

Other names

alisertib plus endocrine therapyalisertib in combination with endocrine therapy